Theophylline (1,3-Dimethylxanthine) sodium glycinate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline sodium glycinate inhibits PDE3 activity to relax airway smooth muscle. Theophylline sodium glycinate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline sodium glycinate induces apoptosis. Theophylline sodium glycinate can be used for asthma and chronic obstructive pulmonary disease (COPD) research[1][2][3][4][5].
A2B receptor antagonist 1 is a potent A2B adenosine receptor antagonist extracted from patent WO 2009157938 A1 EXAMPLE 9B.
SCH-202676 hydrobromide is an allosteric modulator of G protein-coupled receptors (GPCRs) and adenosine receptor (AR). SCH-202676 hydrobromide has antiviral activity and inhibits 3CLpro in a time-dependent manner with an IC50 value of 0.655 μM[1][2][3][4].
LUF6000 is an allosteric modulator of the human A3 adenosine receptor (AR). IC50 value: Target: A3 adenosine receptor LUF6000 was found to be an allosteric enhancer of Emax of structurally diverse agonists at the A3 AR, being more effective for low-Emax agonists than for high-Emax agonists. LUF6000 exerted an Emax-enhancing effect at a concentration of 0.1 microM or higher, and was shown to increase the Emax of Cl-IB-MECA and other low-efficacy agonists to a larger extent than that of the high-efficacy agonist NECA. Interestingly, LUF6000 converted a nucleoside A3 AR antagonist MRS542, but not a non-nucleoside antagonist MRS1220, into an agonist.
CGS 21680 is a specific adenosine A2A receptor agonist, used for treatment of neurological disease.
A1AR antagonist 6 (compound 15) is a potent and selective A1AR (A1 adenosine receptor) antagonist, with a pIC50 of 6.38 and a pKi of 7.13[1].
Adenosine antagonist-1 is an adenosine A3 receptor (AA3R) antagonist.
BAY-545 is a potent and selective A2B adenosine receptor antagonist, with an IC50 of 59 nM. BAY-545 also exhibits IC50s of 66, 400, 280 nM for human, mouse, rat A2B adenosine receptor in cells, respectively, and a Ki of 97 nM for human A2B adenosine receptor, with more selectivity over A1, A2A, and A3 adenosine receptor[1].
CGS 21680 Hydrochloride is a selective adenosine A2A receptor agonist with a Ki of 27 nM.
Istradefylline-13C,d3 is the 13C- and deuterium labeled. Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
Adenosine receptor antagonist 2 is an orally active A2a/A2b adenosine receptor antagonist with IC50s of 1 nM and 3 nM, respectively. Adenosine receptor antagonist 2 has anti-tumor activity[1].
CPI-444 is a potent and selective inhibitor of A2A receptor (A2AR) induces antitumor responses.
Vipadenant is an adenosine receptor antagonist, with Kis of 1.3 nM and 68 nM for A2A and A1, respectively.
UP202-56 is an adenosine analogue, which is an adenosinergic agonist.
CV1808 (2-Phenylaminoadenosine) is a non-selective A2 adenosine receptor (A2 AR) agonist with Kis of 76 and 1450 nM for A2A and A3 adenosine receptor subtypes, respectively[1].
Piclidenoson (IB-MECA) is an agonist of the adenosine A3 receptor with EC50 values of 0.11 μM. IC50 value: 0.11 μM (EC50) [3]Target: adenosine A3 receptorin vitro: Piclidenoson has been shown to play important roles in cell proliferation and apoptosis in a variety of cancer cell lines. ThePiclidenoson was capable of decreasing intracellular cyclic adenosine monophosphate (cAMP) that was the reason for the presence of functional A3 adenosine receptor on the cell lines. Piclidenoson significantly reduced cell viability in a dose-dependent manner. Piclidenoson, an A3AR agonist, inhibits the growth of different cancer cell types like melanoma, colon, breast, leukemia, and prostatePiclidenoson was able to inhibit forskolin-stimulated cAMP levels with an EC50 value of 0.82 μM in OVCAR-3 cells. Piclidenoson was able to inhibit forskolin-stimulated cAMP levels with an EC50 value of 1.2 μM in Caov-4 cells.in vivo: Administrations of single intraperitoneal doses of either Piclidenoson 0.5 h post-irradiation resulted in statistically significant increases of MST in comparison with the control irradiated mice.[2]
SDZ-WAG994 (WAG-994) is a stable, long-acting, selective and orally active A1-adenosine receptor agonist with a KD of 23 nM. SDZ-WAG994 can be used for the research of atrial fibrillation[1].
Preladenant is a potent and competitive antagonist of the human adenosine A2A receptor with a Ki of 1.1 nM and has over 1000-fold selectivity over other adenosine receptors.
Binodenoson (MRE-0470) is a potent and selective A2A adenosine receptor agonist (KD=270 nM). Binodenoson is being developed as a short-acting coronary vasodilator as an adjunct to radiotracers for use in myocardial stress imaging[1].
Doxofylline is an antagonist of adenosine A1 receptor which also inhibits phosphodiesterase IV.
MRS 1754 is a selective antagonist radioligand for A2B adenosine receptor with very low affinity for A1 and A3 receptors of both humans and rats[1].
Namodenoson (CF-102) is a selective A3 adenosine receptor agonist (Ki = 0.33 nM). Displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively.
Adenosine A1 receptor activator T62 is an allosteric enhancer of adenosine A1 receptor. Adenosine A1 receptor activator T62 produces antinociception in animal models of acute pain and also reduces hypersensitivity in models of inflammatory and nerve-injury pain[1][2][3].
A2A receptor antagonist 3 (Example 92) is an adenosine A2a receptor antagonist with a Ki of 0.4 nM. A2A receptor antagonist 3 also binds to A2b, A1 and A3 receptor with Kis of 37, 107 and 1467 nM, respectively[1].
5'-N-Ethylcarboxamidoadenosine (NECA) is a nonselective adenosine receptor agonist.
MRS-1706 is a potent and selective A(2B) adenosine receptor antagonist with a Ki value of 1.39 nM.
Norisoboldine hydrochloride is an orally active natural aryl hydrocarbon receptor (AhR) agonist. Norisoboldine hydrochloride, as a major isoquinoline alkaloid present in Radix Linderae, can be used for the research of Rheumatoid arthritis and Ulcerative colitis[1][2].
GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM)[1]. GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse[2]. GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice[3].
MRE3008F20 is a highly potent and selective antagonistic of adenosine A3 receptor (AA3R), inhibits agonist-induced cAMP elevation in resting T lymphocytes with an IC50 of 5 nM[1].